Semlali Abdelhabib, Beji Sarra, Ajala Ikram, Al-Zharani Mohammed, Rouabhia Mahmoud
Groupe de Recherche en Écologie Buccale, Faculté de Médecine Dentaire, Université Laval, Québec, QC G1V0A6, Canada.
Biology Department, College of Science, Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh 11623, Saudi Arabia.
Curr Issues Mol Biol. 2023 Jun 8;45(6):5018-5035. doi: 10.3390/cimb45060319.
Oral cancer has traditionally been treated with surgery, radiotherapy, chemotherapy, or a combination of these therapies. Although cisplatin, a chemotherapy drug, can effectively kill oral cancer cells by forming DNA adducts, its clinical use is limited due to adverse effects and chemo-resistance. Therefore, there is a need to develop new, targeted anticancer drugs to complement chemotherapy, allowing for reduced cisplatin doses and minimizing adverse effects. Recent studies have shown that 3,5-Bis (4-hydroxy-3-methoxybenzylidene)-N-methyl-4-piperidine (PAC), a new curcumin analog, possesses anticancer properties and could be considered a complementary or alternative therapy. In this study, we aimed to assess the potential complementary effects of PAC in combination with cisplatin for treating oral cancer. We conducted experiments using oral cancer cell lines (Ca9-22) treated with different concentrations of cisplatin (ranging from 0.1 μM to 1 μM), either alone or in conjunction with PAC (2.5 and 5 μM). Cell growth was measured using the MTT assay, while cell cytotoxicity was evaluated using an LDH assay. Propidium iodide and annexin V staining were employed to examine the impact on cell apoptosis. Flow cytometry was used to investigate the effects of the PAC/cisplatin combination on cancer cell autophagy, oxidative stress, and DNA damage. Additionally, a Western Blot analysis was performed to assess the influence of this combination on pro-carcinogenic proteins involved in various signaling pathways. The results demonstrated that PAC enhanced the efficacy of cisplatin in a dose-dependent manner, leading to a significant inhibition of oral cancer cell proliferation. Importantly, treatment with PAC (5 μM) alongside different concentrations of cisplatin reduced the IC50 of cisplatin tenfold. Combining these two agents increased apoptosis by further inducing caspase activity. In addition, the concomitant use of PAC and cisplatin enhances oral cancer cell autophagy, ROS, and MitoSOX production. However, combined PAC with cisplatin inhibits the mitochondrial membrane potential (ΔΨm), which is a marker for cell viability. Finally, this combination further enhances the inhibition of oral cancer cell migration via the inhibition of epithelial-to-mesenchymal transition genes, such as E-cadherin. We demonstrated that the combination of PAC and cisplatin markedly enhanced oral cancer cell death by inducing apoptosis, autophagy, and oxidative stress. The data presented indicate that PAC has the potential to serve as a powerful complementary agent to cisplatin in the treatment of gingival squamous cell carcinomas.
口腔癌传统上通过手术、放疗、化疗或这些疗法的联合进行治疗。尽管化疗药物顺铂可通过形成DNA加合物有效杀死口腔癌细胞,但其临床应用因不良反应和化疗耐药性而受到限制。因此,需要开发新的靶向抗癌药物来补充化疗,从而减少顺铂剂量并将不良反应降至最低。最近的研究表明,新型姜黄素类似物3,5-双(4-羟基-3-甲氧基亚苄基)-N-甲基-4-哌啶(PAC)具有抗癌特性,可被视为一种补充或替代疗法。在本研究中,我们旨在评估PAC与顺铂联合治疗口腔癌的潜在协同作用。我们使用不同浓度(0.1 μM至1 μM)的顺铂单独或与PAC(2.5 μM和5 μM)联合处理口腔癌细胞系(Ca9-22)进行实验。使用MTT法测量细胞生长,同时使用LDH法评估细胞毒性。采用碘化丙啶和膜联蛋白V染色来检测对细胞凋亡的影响。使用流式细胞术研究PAC/顺铂联合用药对癌细胞自噬、氧化应激和DNA损伤的影响。此外,进行蛋白质免疫印迹分析以评估这种联合用药对参与各种信号通路的促癌蛋白的影响。结果表明,PAC以剂量依赖的方式增强了顺铂的疗效,导致口腔癌细胞增殖受到显著抑制。重要的是,用PAC(5 μM)与不同浓度的顺铂联合处理使顺铂的半数抑制浓度(IC50)降低了十倍。联合使用这两种药物通过进一步诱导半胱天冬酶活性增加了细胞凋亡。此外,PAC与顺铂联合使用可增强口腔癌细胞的自噬、活性氧(ROS)和MitoSOX生成。然而,PAC与顺铂联合使用会抑制线粒体膜电位(ΔΨm),这是细胞活力的一个指标。最后,这种联合用药通过抑制上皮-间质转化基因(如E-钙黏蛋白)进一步增强了对口腔癌细胞迁移的抑制作用。我们证明,PAC与顺铂联合使用通过诱导细胞凋亡、自噬和氧化应激显著增强了口腔癌细胞死亡。所呈现的数据表明,PAC有潜力在牙龈鳞状细胞癌的治疗中作为顺铂的有力补充剂。
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